Antiprotozoal effects

Mecfianism of Action An anti-infective that interferes with nuclear metabolism and incorporation of nucleotides, inhibiting DNA, RNA, phospholipid, and protein synthesis, THerapeutic Effect Produces antibacterial and ID-antiprotozoal effects, Pfiarmacokinetics Well absorbed after IM administration minimally absorbed after inhalation. Widely distributed. Primarily excreted in urine. Minimally removed by hemodialysis, Half-life 6,5 hr (increased in impaired renal function). 

Mecfianism of Action A nitroimidazole derivative that is converted to the active metabolite by reduction of cell extracts otTricfiomonas. The active metabolite causes DNA damage in pathogens. Therapeutic Effect Produces antiprotozoal effect. Pharmacokinetics Rapidly and completely absorbed. Protein binding 12%. Distributed in all bodytissues and fluids crosses blood-brain barrier. Significantly metabolized. Primarily excreted in urine partially eliminated in feces. Half-life 12-14 hr. 

Answer C. In amebic dysentery caused by Entamoeba histolytica and GI infections with diarrhea ( back-packer s diarrhea ) due to Giardia lamblia, metronidazole is the drug of choice. Diloxanide is a backup drug for noninvasive intestinal amebiasis, but it has minimal activity in giardial infections. Quinacrine has effectiveness in giardiasis but not amebiasis. TMP-SMX has antiprotozoal effectiveness in Pneumocystis carinii pneumonia. Ciprofloxacin is devoid of antiprotozoal activity. 

As stated above, it is of crucial importance to distinguish specific antiprotozoal effects from non-specific cytotoxicity. It is certainly possible to do so for individual compounds, e.g. by calculating the ratio of IC50 values for antiprotozoal and for cytotoxic activity as was done e.g. in [77, 78], On the other hand, it has been demonstrated that cytotoxicity data for STLs vs. different cell lines do not necessarily... 

ANTIPROTOZOAL EFFECTS Melarsoprol is a prodrug that is metabolized rapidly (t j of 30 minutes) to melarsen oxide, the active form. Arsenoxides react avidly and reversibly with sulfhydryl groups and thereby inactivate many enzymes. Melarsoprol reacts with trypanothione to form melarsen oxide-trypanothione adduct, which potently inhibits trypanothione reductase. Both the sequestering of trypanothione and the inhibition of trypanothione reductase are expected to have lethal consequences to the cell, but this remains unproven. 

ANTIPROTOZOAL EFFECTS Miltefosine is the first orally available therapy for leishmaniasis. It is safe and effective treatment for visceral leishmaniasis and has also shown >95% efficacy against cutaneous leishmaniasis. In Leishmania, the drug may alter ether-lipid metabohsm, ceU signaling, or glycosylphosphatidylinosital anchor biosynthesis. Mutations in a P-type ATPase of the aminophospholipid translocase subfamily apparently decrease drug uptake and thereby confer resistance. 

ANTIPROTOZOAL EFFECTS Nifurtimox and benznidazole are trypanocidal against both the trypomastigote and amastigote forms of T. cruzi. Nifurtimox also has activity against T. brucei and can cure early- and late-stage disease. 

ANTIPROTOZOAL EFFECTS The diamidines are effective for the treatment of T. brucei gambiense sleeping sickness but not T. brucei rhodesiense or T. cruzi infections. They also are useful for treating antimony-resistant leishmaitia. 

A. annua has been found to produce two antiparasitic methoxylated flavones, artemetin and casticin (Fig. 9). Extracts from Artemisia absinthium have been also reported to have antiprotozoal effects against Trypanosoma brucei. Trypanosoma cruzi, and Leishmania infantum [102],... 

Examples of Recent Research into the Antiprotozoal Effects of Essential Oils... 

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